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Elacestrant is an oral selective estrogen receptor degrader (SERD).
1. Common name : Elacetrant
< b>2. Trade name : ORSERDU™
3. Dosage form : Oral film-coated tablets
4. Main ingredient u200 c: Each tablet contains 345 mg or 86 mg of elastran (corresponding to 400 mg and 100 mg of ilagrastat dihydrochloride respectively)
5. Excipient : Colloidal dioxygen Silicone, crospovidone, magnesium stearate (not of animal origin), microcrystalline cellulose, silicified microcrystalline cellulose, Opadry II Blue (polyvinyl alcohol, titanium dioxide, polyethylene glycol, FD&C Blue No. 1, talc).
ER-positive/HER2-negative, ESR1-mutated breast cancer : used to treat postmenopausal women or adult men with ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer, and the disease has progressed after at least first-line endocrine therapy.
1. Specifications :
345 mg tablet: light blue unscored oval biconvex tablet, with "MH" printed on one side.
86 mg tablet: light blue non-scored round biconvex tablet with “ME” printed on one side.
2. Packaging : 30 pieces per bottle, child-safe cap.
1. Recommended dosage of : 345mg once a day, taken with food (to reduce the risk of nausea and vomiting), swallow the tablet whole, do not chew, crush or split.
2. Missing a dose or vomiting : If you miss a dose for more than 6 hours or vomit after taking the medicine, skip the dose and take it at the original planned time the next day.
3. Dose adjustment of :
First dose reduction of : 258mg/day (3 tablets of 86mg);
Second dose reduction of : 172mg/day (2 tablets of 86mg);
If further reduction is required, the drug will be permanently discontinued.
Liver injury : reduce the dose to 258mg/day for moderate (Child-PughB) and disabled for severe (Child-PughC).
1. Diet : It needs to be taken with meals to reduce gastrointestinal reactions.
2. Monitor : Check blood lipids (cholesterol, triglycerides), liver function (ALT/AST) and blood sodium levels regularly before and during treatment.
3. Drug interaction :
Avoid the combined use of strong/moderate CYP3A4 inhibitors (such as itraconazole) or inducers (such as rifampicin).
The dose of P-gp/BCRP substrates (such as digoxin and rosuvastatin) needs to be reduced.
1. Pregnant women : Contraindicated, may cause fetal malformations (animal data show embryotoxicity).
2. Lactation : Breastfeeding is prohibited during treatment and within 1 week after the last dose.
3. Family planning :Patients of childbearing age need to take effective contraceptive measures (during treatment and 1 week after stopping medication).
4. U200c for the elderly: No dose adjustment is required, but close monitoring is required.
1. Common (>10%) : Musculoskeletal pain (41%), nausea (35%), high cholesterol (30%), high triglycerides (27%), fatigue (26%), vomiting (19%), diarrhea (13%), headache (12%).
2. Serious but rare : Hepatotoxicity (ALT/AST elevation), venous thrombosis (6%), embryo-fetal toxicity.
There are no absolute contraindications, but it is contraindicated in patients with severe liver damage (Child-PughC).
1. CYP3A4 affects : Strong inhibitors (such as clarithromycin) increase the exposure of elastran by 5.3 times, and strong inducers (such as rifampicin) reduce the exposure by 86%.
2. P-gp/BCRP inhibits : It may increase the plasma concentration of digoxin, rosuvastatin and other drugs.
Save at room temperature (20-25°C), allow short-term exposure to 15-30°C, avoid light and moisture.
Note : If you have persistent nausea, jaundice or muscle pain during medication, you need to seek medical treatment in time. Specific medication needs to be combined with the results of ESR1 mutation testing.